Fluoro-benzimidazole derivatives to cure Alzheimer's disease: In-silico studies, synthesis, structure-activity relationship and in vivo evaluation for β secretase enzyme inhibition.
Sayyad Ali et al.
Bioorganic chemistry, 88, 102936-102936 (2019-05-06)
Lu Zhao et al.
Cells, 8(5) (2019-05-22)
β-site APP-cleaving enzyme 1 (BACE1) initiates amyloid precursor protein (APP) cleavage and β-amyloid (Aβ) production, a critical step in the pathogenesis of Alzheimer's disease (AD). It is thus of considerable interest to investigate how BACE1 activity is regulated. BACE1 has...
L Hong et al.
Biochemical Society transactions, 30(4), 530-534 (2002-08-28)
As beta-secretase, memapsin 2 cleaves amyloid-beta precursor protein, which leads ultimately to the onset of Alzheimer's disease. As such, memapsin 2 is an excellent target of inhibitor drugs for the treatment of this disease. Here we describe the tools for...
Lucas J Gutierrez et al.
Journal of biomolecular structure & dynamics, 35(2), 413-426 (2016-01-28)
We report here two new small-size peptides acting as modulators of the β-site APP cleaving enzyme 1 (BACE1) exosite. Ac-YPYFDPL-NH2 and Ac-YPYDIPL-NH2 displayed a moderate but significant inhibitory effect on BACE1. These peptides were obtained from a molecular modeling study....
Vijay K Nuthakki et al.
Drug development research, 80(5), 655-665 (2019-05-03)
Beta-secreatse (BACE-1) and cholinesterases are clinically validated targets of Alzheimer's disease (AD), for which natural products have provided immense contribution. The multifaceted nature of AD signifies the need of multitargeted agents to tackle this disease. In the search of new...